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Heteroarylmethyl amides

a technology of heteroarylmethyl amide and amide, which is applied in the field of heteroarylmethyl amide compounds, can solve the problems of reducing compliance, not having wholly satisfactory hdl-elevating therapies, and significantly elevating plasma hdl levels

Inactive Publication Date: 2012-03-15
F HOFFMANN LA ROCHE INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

No wholly satisfactory HDL-elevating therapies exist.
Niacin can significantly increase HDL, but has serious toleration issues which reduce compliance.
As a result, there is a significant unmet medical need for a well tolerated agent which can significantly elevate plasma HDL levels.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example c1

[0230]Film coated tablets containing the following ingredients can be manufactured in a conventional manner:

IngredientsPer tabletKernel:Compound of formula (I)10.0mg200.0mgMicrocrystalline cellulose23.5mg43.5mgLactose hydrous60.0mg70.0mgPovidone K3012.5mg15.0mgSodium starch glycolate12.5mg17.0mgMagnesium stearate1.5mg4.5mg(Kernel Weight)120.0mg350.0mgFilm Coat:Hydroxypropyl methyl cellulose3.5mg7.0mgPolyethylene glycol 60000.8mg1.6mgTalc1.3mg2.6mgIron oxide (yellow)0.8mg1.6mgTitan dioxide0.8mg1.6mg

[0231]The active ingredient is sieved and mixed with microcrystalline cellulose and the mixture is granulated with a solution of polyvinylpyrrolidone in water. The granulate is then mixed with sodium starch glycolate and magnesium stearate and compressed to yield kernels of 120 or 350 mg respectively. The kernels are lacquered with an aq. solution / suspension of the above mentioned film coat.

example c2

[0232]Capsules containing the following ingredients can be manufactured in a conventional manner:

IngredientsPer capsuleCompound of formula (I)25.0 mgLactose150.0 mgMaize starch20.0 mgTalc5.0 mg

[0233]The components are sieved and mixed and filled into capsules of size 2.

example c3

[0234]Injection solutions can have the following composition:

Compound of formula (I)3.0 mgPolyethylene glycol 400150.0mgAcetic acidq.s. ad pH5.0Water for injection solutionsad 1.0ml

[0235]The active ingredient is dissolved in a mixture of Polyethylene glycol 400 and water for injection (part). The pH is adjusted to 5.0 by addition of acetic acid. The volume is adjusted to 1.0 ml by addition of the residual amount of water. The solution is filtered, filled into vials using an appropriate overage and sterilized.

Pharmacological Tests

[0236]The following tests were carried out in order to determine the activity of the compounds of formula I and their valuable pharmacological properties.

Detection of Upregulation of ABCA1 Protein in Cells

[0237]The ability of compounds of the invention to increase the level of ABCA1 protein is determined in replicate cultures of THP-1 macrophage cells in 96-well microplates. Cells are plated at an initial density of 100,000 cells / well in 100 μl medium and di...

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Abstract

The present invention relates to compounds of the formulawherein A1, A2, A3 and R1 to R8 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and / or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.

Description

PRIORITY TO RELATED APPLICATIONS[0001]This application claims the benefit of European Patent Application No. 10175984.3, filed Sep. 9, 2010, which is hereby incorporated by reference in its entirety.FIELD OF THE INVENTION[0002]The present invention is concerned with heteroarylmethyl amide compounds as HDL-cholesterol raising agents, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The compounds of the present invention can be used in the therapeutic and / or prophylactic treatment of diseases and disorders such as dyslipidemia, atherosclerosis and cardiovascular diseases.BACKGROUND OF THE INVENTION[0003]Atherosclerosis and its associated coronary heart disease are the leading cause of death in the industrialized world. Risk for development of coronary heart disease has been shown to be strongly correlated with certain plasma lipid levels. Lipids are transported in the blood by lipoproteins. The general structure of lipo...

Claims

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Application Information

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IPC IPC(8): A61K31/501C07D417/12C07D401/12A61P9/10C07D239/34A61K31/444A61K31/506C07D413/12C07D239/02
CPCC07D213/82C07D401/12C07D417/12C07D413/14C07D413/12A61P3/04A61P3/06A61P3/10A61P9/00A61P9/10A61P9/12
Inventor HEBEISEN, PAULMATILE, HUGUESROEVER, STEPHANWRIGHT, MATTHEWJENSEN, SANNAH ZOFFMANN
Owner F HOFFMANN LA ROCHE INC
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